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AM679

AM679

产品编号 T14205   CAS 1206880-66-1

AM679 is a potent and selective FLAP inhibitor with IC50s of 2.2 nM/0.6 nM/154 nM for FLAP binding/hLA/hWB respectively. IC50 value: 2.2 nM/0.6 nM/154 nM(FLAP binding/hLA/hWB) [1] AM679 showed an improved CYP inhibition profile (IC50 3A4 = 16.7 lM, 2C9 = 3.7 lM, 2D6 <30 lM), no time dependent inhibition against CYP3A4 (0.003 min-1 vs 0.057 min-1 for troleandomycin control 10 uM) and no CYP3A4 induction. AM679 has an excellent hWB IC50 potency of 154 nM. Target: FLAP in vitro: AM679 showed excellent in vitro inhibition against FLAP. in vivo: AM679 was profiled in a rodent bronchoalveolar lavage (BAL) model to measure its ability to inhibit production of leukotrienes in vivo. 16 Oral administration of 39 (10 mg/kg as the sodium carboxylate salt) 4 h prior to ionophore challenge reduced LTB4 and CysLT levels in the rodent lung lavage fluid by 98% and 87%, respectively, with corresponding average rodent plasma levels of 605 nM (3 h post dose, rat blood LTB4 IC50 = 125 nM).

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AM679 Chemical Structure
AM679, CAS 1206880-66-1
规格 价格/CNY 货期 数量
5 mg ¥ 1,990 5日内发货
50 mg ¥ 6,990 5日内发货
100 mg ¥ 10,800 5日内发货
其他形式的 AM679:
药物设计专题培训
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
产品目录号及名称: AM679 (T14205)
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参考文献
产品描述 AM679 is a potent and selective FLAP inhibitor with IC50s of 2.2 nM/0.6 nM/154 nM for FLAP binding/hLA/hWB respectively. IC50 value: 2.2 nM/0.6 nM/154 nM(FLAP binding/hLA/hWB) [1] AM679 showed an improved CYP inhibition profile (IC50 3A4 = 16.7 lM, 2C9 = 3.7 lM, 2D6 >30 lM), no time dependent inhibition against CYP3A4 (0.003 min-1 vs 0.057 min-1 for troleandomycin control 10 uM) and no CYP3A4 induction. AM679 has an excellent hWB IC50 potency of 154 nM. Target: FLAP in vitro: AM679 showed excellent in vitro inhibition against FLAP. in vivo: AM679 was profiled in a rodent bronchoalveolar lavage (BAL) model to measure its ability to inhibit production of leukotrienes in vivo. 16 Oral administration of 39 (10 mg/kg as the sodium carboxylate salt) 4 h prior to ionophore challenge reduced LTB4 and CysLT levels in the rodent lung lavage fluid by 98% and 87%, respectively, with corresponding average rodent plasma levels of 605 nM (3 h post dose, rat blood LTB4 IC50 = 125 nM).
分子量 692.87
分子式 C40H44N4O5S
CAS No. 1206880-66-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 100 mg/mL (144.33 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.4433 mL 7.2164 mL 14.4327 mL 36.0818 mL
5 mM 0.2887 mL 1.4433 mL 2.8865 mL 7.2164 mL
10 mM 0.1443 mL 0.7216 mL 1.4433 mL 3.6082 mL
20 mM 0.0722 mL 0.3608 mL 0.7216 mL 1.8041 mL
50 mM 0.0289 mL 0.1443 mL 0.2887 mL 0.7216 mL
100 mM 0.0144 mL 0.0722 mL 0.1443 mL 0.3608 mL

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TargetMol Library Books参考文献

1. Stock, N, et al. 5-Lipoxygenase-activating protein inhibitors. Part 2: 3-{5-((S)-1-Acetyl-2,3-dihydro-1H-indol-2-ylmethoxy)-3-tert-butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-1H-indol-2-yl}-2,2-dimethyl-propionic acid (AM679)-A potent FLAP inhib 2. Musiyenko, A, et al. A novel 5-lipoxygenase-activating protein inhibitor, AM679, reduces inflammation in the respiratory syncytial virus-infected mouse eye. Clinical and Vaccine Immunology (2009), 16(11), 1654-1659.

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体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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Keywords

AM679 1206880-66-1 Others AM 679 AM-679 Inhibitor inhibitor inhibit

 

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